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GABA receptors are classified into GABAA receptors which are ligand-gated ion channels (or ionotropic receptors) and GABAB receptors, which are G protein-coupled receptors (metabotropic receptors). GABAA receptors are members of the Cys-loop family that also include the nicotinic acetylcholine, 5-HT3 and strychnine-sensitive glycine receptors. GABAA receptors exist as pentamers of 4TM subunits that form an intrinsic anion selective channel. Sequences of six α, three β, three γ, one δ, three ρ, one ε, one π and one θ GABAA receptor subunits have been reported in mammals. Receptors formed from ρ-subunits have a distinctive pharmacology (eg.insensitivity to bicuculline, benzodiazepines and barbiturates), and have sometimes been termed GABAC receptors. However they are now classified as GABAA receptors ( GABAA-ρ subclass) by NC-IUPHAR, based on structural and functional criteria. GABAB receptors are G protein-coupled receptors that are composed of GABAB1 and GABAB2 subunits, which form the core of the receptor, and auxiliary K-channel tetramerization domain (KCTD) subunits.

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